C07J75/00

METHODS FOR CONVENIENT ASYMMETRIC SYNTHESIS OF C9-SUBSTITUTED STEROID-LIKE COMPOUNDS
20240182516 · 2024-06-06 ·

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds. In one aspect, the present disclosure relates to preparing a C9-alpha-substituted or a C9-beta-substituted compound (steroid numbering), the method comprising the steps of providing a tertiary allylic substrate and performing a regio- and stereoselective cyclization reaction to form a C9-C10 bond and to set a quaternary center at C9.

COMPLEX AND STRUCTURALLY DIVERSE COMPOUNDS

The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

PREPARATION OF BILE ACIDS AND INTERMEDIATES THEREOF

Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

PREPARATION OF BILE ACIDS AND INTERMEDIATES THEREOF

Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

EXTRACTION OF PHYTOSTEROLS FROM TALL OIL SOAP USING A SOLVENT SELECTED FROM DIBROMOMETHANE, BROMOFORM, TETRABROMOMETHANE OR A COMBINATION THEREOF
20190010420 · 2019-01-10 · ·

The present invention relates to extraction of phytosterols from alkaline tall oil soap which is obtained from the Kraft process black liquor by skimming. In the method according to the present invention, phytosterols are extracted using dibromomethane, bromoform, tetrabromomethane or a combination thereof.

EXTRACTION OF PHYTOSTEROLS FROM TALL OIL SOAP USING A SOLVENT SELECTED FROM DIBROMOMETHANE, BROMOFORM, TETRABROMOMETHANE OR A COMBINATION THEREOF
20190010420 · 2019-01-10 · ·

The present invention relates to extraction of phytosterols from alkaline tall oil soap which is obtained from the Kraft process black liquor by skimming. In the method according to the present invention, phytosterols are extracted using dibromomethane, bromoform, tetrabromomethane or a combination thereof.

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Compounds are provided according to Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):

##STR00002##

and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

Methods for assembly of tetracyclic compounds by stereoselective C9-C10 bond formation
12065465 · 2024-08-20 · ·

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

Process for the preparation of 17-desoxy-corticosteroids

The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

Process for the preparation of 17-desoxy-corticosteroids

The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.